[go: up one dir, main page]
More Web Proxy on the site http://driver.im/

CA2883894A1 - Composes et procedes pour la modulation des kinases, et leurs indications - Google Patents

Composes et procedes pour la modulation des kinases, et leurs indications Download PDF

Info

Publication number
CA2883894A1
CA2883894A1 CA2883894A CA2883894A CA2883894A1 CA 2883894 A1 CA2883894 A1 CA 2883894A1 CA 2883894 A CA2883894 A CA 2883894A CA 2883894 A CA2883894 A CA 2883894A CA 2883894 A1 CA2883894 A1 CA 2883894A1
Authority
CA
Canada
Prior art keywords
substituents
optionally substituted
compound
ring
nhc
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
CA2883894A
Other languages
English (en)
Other versions
CA2883894C (fr
Inventor
Jack Lin
John BUELL
Katrina Chan
Todd Ewing
Prabha N. Ibrahim
Marika Nespi
Phuongly Pham
Songyuan Shi
Wayne Spevak
Guoxian Wu
Jiazhong Zhang
Ying Zhang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Plexxikon Inc
Original Assignee
Plexxikon Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Plexxikon Inc filed Critical Plexxikon Inc
Publication of CA2883894A1 publication Critical patent/CA2883894A1/fr
Application granted granted Critical
Publication of CA2883894C publication Critical patent/CA2883894C/fr
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/74Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • C07D491/056Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

L'invention concerne des composés actifs sur les protéine kinases c-kit ou les protéine kinases c-kit mutantes ayant des mutations quelconques, ainsi que des procédés de préparation et d'utilisation de ces composés pour traiter des maladies et des affections associées à une activité aberrante des protéine kinases c-kit et des protéine kinases c-kit mutantes.
CA2883894A 2012-09-06 2013-09-05 Composes et procedes pour la modulation des kinases, et leurs indications Active CA2883894C (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261697761P 2012-09-06 2012-09-06
US61/697,761 2012-09-06
US201361775347P 2013-03-08 2013-03-08
US61/775,347 2013-03-08
PCT/US2013/058320 WO2014039714A2 (fr) 2012-09-06 2013-09-05 Composés et procédés pour la modulation des kinases, et leurs indications

Publications (2)

Publication Number Publication Date
CA2883894A1 true CA2883894A1 (fr) 2014-03-13
CA2883894C CA2883894C (fr) 2020-08-18

Family

ID=50237764

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2883894A Active CA2883894C (fr) 2012-09-06 2013-09-05 Composes et procedes pour la modulation des kinases, et leurs indications

Country Status (9)

Country Link
US (1) US10227357B2 (fr)
EP (1) EP2892534B8 (fr)
JP (1) JP6318156B2 (fr)
CN (1) CN104981247A (fr)
AU (1) AU2013312477B2 (fr)
CA (1) CA2883894C (fr)
ES (1) ES2889757T3 (fr)
MX (1) MX2015002887A (fr)
WO (1) WO2014039714A2 (fr)

Families Citing this family (102)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008063888A2 (fr) 2006-11-22 2008-05-29 Plexxikon, Inc. Composés modulant l'activité de c-fms et/ou de c-kit et utilisations associées
AU2008276063B2 (en) 2007-07-17 2013-11-28 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
WO2009143018A2 (fr) 2008-05-19 2009-11-26 Plexxikon, Inc. Composés et procédés de modulation des kinases, et indications associées
KR20120097512A (ko) 2009-11-18 2012-09-04 플렉시콘, 인코퍼레이티드 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증
AU2010336524B2 (en) 2009-12-23 2015-10-08 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
TWI619713B (zh) 2010-04-21 2018-04-01 普雷辛肯公司 用於激酶調節的化合物和方法及其適應症
JP5927201B2 (ja) 2010-12-16 2016-06-01 カルチャン リミテッド Ask1阻害ピロロピリミジン誘導体
EA028821B9 (ru) 2011-02-07 2018-10-31 Плексксикон, Инк. Соединения и способы для модуляции киназ, а также показания к их применению
BR112013029163A2 (pt) 2011-05-17 2017-01-31 Plexxikon Inc modulação quinase e indicações dos mesmos
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
PT2935248T (pt) 2012-12-21 2018-04-05 Plexxikon Inc Compostos e métodos para a modulação de quinase e indicações associadas
ES2746756T3 (es) 2013-03-11 2020-03-06 Merck Patent Gmbh Derivados de 6-[4-(1H-imidazol-2-il)piperidin-1-il]pirimidin-4-amina como moduladores de la actividad cinasa
AU2014233437B2 (en) 2013-03-15 2018-07-26 Opna Immuno Oncology, SA Heterocyclic compounds and uses thereof
WO2014160521A1 (fr) 2013-03-15 2014-10-02 Blueprint Medicines Corporation Dérivés de pipérazine et leur utilisation comme modulateurs de kit
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
DE102013008118A1 (de) 2013-05-11 2014-11-13 Merck Patent Gmbh Arylchinazoline
EP3004060B1 (fr) * 2013-05-30 2019-11-27 Plexxikon Inc. Composés pour modulation de kinases, et indications correspondantes
SG11201602937UA (en) 2013-10-17 2016-05-30 Blueprint Medicines Corp Compositions useful for treating disorders related to kit
US9334263B2 (en) 2013-10-17 2016-05-10 Blueprint Medicines Corporation Compositions useful for treating disorders related to kit
TN2016000227A1 (fr) 2013-12-05 2017-10-06 Pfizer Pyrrolo[2,3-d]pyrimidinyle, pyrrolo[2,3-b]pyrazinyle et pyrollo[2,3-d]pyridinyle acrylamides.
US9771369B2 (en) 2014-03-04 2017-09-26 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
GB201410816D0 (en) * 2014-06-17 2014-07-30 Ucb Biopharma Sprl And Katholieke Universiteit Leuven Therapeutic agents
WO2016044067A1 (fr) 2014-09-15 2016-03-24 Plexxikon Inc. Composés hétérocycliques et leurs utilisations
EP3798214B1 (fr) 2014-10-06 2022-09-14 Vertex Pharmaceuticals Incorporated Modulateurs de régulateur de conductance transmembranaire de la fibrose kystique
WO2016164641A1 (fr) 2015-04-08 2016-10-13 Plexxikon Inc. Composés et méthodes de modulation des kinases, et leurs indications
EP3581573B1 (fr) 2015-05-06 2022-07-06 Plexxikon Inc. Synthèse d'un composé modulant des kinases
ES2820827T3 (es) 2015-05-06 2021-04-22 Plexxikon Inc Formas sólidas de un compuesto modulador de quinasas
US10316032B2 (en) 2015-05-22 2019-06-11 Plexxikon Inc. Solid forms of a compound for modulating kinases
WO2017019804A2 (fr) 2015-07-28 2017-02-02 Plexxikon Inc. Composés et procédés de modulation des kinases, et indications associées
WO2017027717A1 (fr) 2015-08-12 2017-02-16 Incyte Corporation Composés de pyrimidine fusionnés bicycliques utilisés en tant qu'inhibiteurs de tam
WO2017035366A1 (fr) * 2015-08-26 2017-03-02 Incyte Corporation Dérivés de type pyrrolo-pyrimidine utilisés comme inhibiteurs des tam
KR20180052757A (ko) 2015-09-21 2018-05-18 플렉시콘 인코퍼레이티드 헤테로시클릭 화합물 및 그의 용도
WO2017100201A1 (fr) 2015-12-07 2017-06-15 Plexxikon Inc. Composés et procédés pour la modulation de kinase, et indications associées
CN105311585A (zh) * 2015-12-08 2016-02-10 李朝彬 一种治疗肝硬化的中药组合物
US9630968B1 (en) 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
CA3017972C (fr) 2016-03-16 2023-03-28 Plexxikon Inc. Composes et procedes de modulation de kinases et indications associees
UA123785C2 (uk) 2016-03-28 2021-06-02 Інсайт Корпорейшн Сполуки піролотриазину як інгібітори tam
CA3019380A1 (fr) 2016-03-31 2017-10-05 Vertex Pharmaceuticals Incorporated Modulateurs du regulateur de la conductance transmembranaire de la fibrose kystique
CN105936633B (zh) * 2016-04-27 2018-11-09 广东环境保护工程职业学院 5-(3-异丙基苯并异噁唑)吡嗪-2-胺及其制备方法
AU2017315343A1 (en) * 2016-08-24 2019-02-28 Arqule, Inc. Amino-pyrrolopyrimidinone compounds and methods of use thereof
TW201815766A (zh) 2016-09-22 2018-05-01 美商普雷辛肯公司 用於ido及tdo調節之化合物及方法以及其適應症
HUE056716T2 (hu) 2016-09-30 2022-03-28 Vertex Pharma Cisztás firbrózis transzmembrán konduktancia regulátor modulátora, gyógyszerészeti készítmények, kezelési eljárások, és eljárások a modulátor elõállítására
DK3551622T3 (da) 2016-12-09 2020-11-23 Vertex Pharma Modulator af transmembrankonduktansregulator af cystisk fibrose, farmaceutiske sammensætninger, behandlingsfremgangsmåder og fremgangsmåde til fremstilling af modulatoren
UA126394C2 (uk) * 2016-12-22 2022-09-28 Інсайт Корпорейшн Похідні бензоксазолу як імуномодулятори
CA3047580A1 (fr) 2016-12-23 2018-07-26 Plexxikon Inc. Composes et procedes pour la modulation de cdk8, et indications associees
ES2896502T3 (es) 2017-03-20 2022-02-24 Plexxikon Inc Formas cristalinas de ácido 4-(1-(1,1-di(piridin-2-il) etil)-6-(3,5-dimetilisoxazol-4-il)-1H-pirrolo[3,2-b]piridin-3- il)benzoico que inhiben el bromodominio
WO2018183712A1 (fr) 2017-03-31 2018-10-04 Blueprint Medicines Corporation Composés de pyrrolo[1,2-b]pyridazine et compositions utiles pour traiter des troubles liés à kit et pdgfr
WO2018226846A1 (fr) 2017-06-07 2018-12-13 Plexxikon Inc. Composés et procédés de modulation de kinase
CA3066084A1 (fr) 2017-06-08 2018-12-13 Vertex Pharmaceuticals Incorporated Methodes de traitement de la fibrose kystique
CA3069226A1 (fr) 2017-07-17 2019-01-24 Vertex Pharmaceuticals Incorporated Methodes de traitement de la fibrose kystique
JP7170030B2 (ja) 2017-07-25 2022-11-11 プレキシコン インコーポレーテッド キナーゼを調節する化合物の製剤
AU2018309043B2 (en) 2017-08-02 2022-03-31 Vertex Pharmaceuticals Incorporated Processes for preparing pyrrolidine compounds
CN109400610A (zh) * 2017-08-18 2019-03-01 浙江海正药业股份有限公司 吡咯并三嗪类衍生物、其制备方法及其在医药上的用途
CR20200179A (es) 2017-09-27 2020-11-02 Incyte Corp Sales de inhibidores de tam
EP3694855A1 (fr) 2017-10-13 2020-08-19 Plexxikon Inc. Formes solides d'un composé pour la modulation de kinases
TWI719349B (zh) 2017-10-19 2021-02-21 美商維泰克斯製藥公司 Cftr調節劑之結晶形式及組合物
EP3700574B1 (fr) 2017-10-27 2024-08-28 Plexxikon Inc. Formulation d'un composé modulant les kinases
AU2018380426B2 (en) 2017-12-08 2023-05-18 Vertex Pharmaceuticals Incorporated Processes for making modulators of cystic fibrosis transmembrane conductance regulator
TWI810243B (zh) 2018-02-05 2023-08-01 美商維泰克斯製藥公司 用於治療囊腫纖化症之醫藥組合物
IL277071B2 (en) 2018-03-08 2024-07-01 Incyte Corp Aminopyrizine diol compounds as PI3K–y inhibitors
AU2019239952A1 (en) 2018-03-20 2020-10-08 Plexxikon Inc. Compounds and methods for IDO and TDO modulation, and indications therefor
WO2019200246A1 (fr) 2018-04-13 2019-10-17 Alexander Russell Abela Modulateurs du régulateur de la conductance transmembranaire de la fibrose kystique, compositions pharmaceutiques, procédés de traitement et procédé de fabrication du modulateur
CN109970745B (zh) 2018-04-16 2020-12-08 深圳市塔吉瑞生物医药有限公司 取代的吡咯并三嗪类化合物及其药物组合物及其用途
WO2019243971A1 (fr) * 2018-06-17 2019-12-26 Foundation For Neglected Disease Research Nouveaux composés et leurs procédés d'utilisation
SG11202013163TA (en) 2018-06-29 2021-01-28 Incyte Corp Formulations of an axl/mer inhibitor
WO2020010003A1 (fr) 2018-07-02 2020-01-09 Incyte Corporation DÉRIVÉS D'AMINOPYRAZINE UTILISÉS EN TANT QU'INHIBITEURS DE PI3K-γ
CN116574105A (zh) * 2018-09-27 2023-08-11 深圳微芯生物科技股份有限公司 具有吲哚胺-2,3-双加氧酶抑制活性的喹啉衍生物
MX2021005875A (es) * 2018-11-20 2021-09-23 Univ Georgetown Composiciones y métodos para el tratamiento de trastornos neurodegenerativos, miodegenerativos y de almacenamiento lisosómico.
CN111410648B (zh) * 2019-01-07 2024-03-29 浙江海正药业股份有限公司 一种手性c-KIT抑制剂药物关键中间体及其制备方法
CN113454082B (zh) 2019-02-22 2024-07-02 第一生物治疗股份有限公司 咪唑并吡啶基化合物及其用于治疗神经退行性疾病的用途
CA3136224A1 (fr) 2019-04-09 2020-10-15 Plexxikon Inc. Azines condensees pour la modulation ep300 ou cbp et indications pour celles-ci
PT3856341T (pt) 2019-04-12 2023-12-12 Blueprint Medicines Corp Formas cristalinas de (s)-1-(4-fluorofenil)-1-(2-(4-(6-(1- metil-1h-pirazol-4-il)pirrolo[2,1-f][1,2,4]triazin-4- il)piperazinil)pirimidin-5-il)etan-1-amina e métodos de preparação
SG11202111244XA (en) 2019-04-12 2021-11-29 Blueprint Medicines Corp Pyrrolotriazine derivatives for treating kit- and pdgfra-mediated diseases
WO2021020902A1 (fr) * 2019-07-30 2021-02-04 주식회사 하임바이오 Nouveau composé anticancéreux et composition pharmaceutique le comprenant en tant que principe actif
CA3163105A1 (fr) 2019-11-28 2021-06-03 Bayer Aktiengesellschaft Aminoquinolones substituees en tant qu'inhibiteurs de dgkalpha pour activation immunitaire
CR20220303A (es) 2019-12-24 2022-09-02 Gilead Sciences Inc Compuestos moduladores de la diacilglicerol quinasa
CN117964757A (zh) 2020-02-14 2024-05-03 吉利德科学公司 与ccr8结合的抗体和融合蛋白及其用途
CN111303155A (zh) * 2020-03-13 2020-06-19 深圳大学 靶向pak1抑制剂及其在抗肿瘤治疗药物中的应用
CN111320634A (zh) * 2020-04-14 2020-06-23 浙江工业大学 一种乙酰氧取代的吡咯并[2,3-d]嘧啶衍生物的制备方法
CA3177522A1 (fr) 2020-04-23 2021-10-28 Opna Immuno-Oncology Sa Composes et procedes de modulation de cd73 et leurs indications
WO2022040512A1 (fr) 2020-08-21 2022-02-24 Plexxikon Inc. Thérapies anticancéreuses à base de médicaments combinatoires
KR102590444B1 (ko) * 2020-10-16 2023-10-18 김홍렬 Pmca 억제제를 포함하는 코로나바이러스 감염 또는 감염 질환의 치료용 조성물
KR102590438B1 (ko) * 2020-10-16 2023-10-18 김홍렬 Pmca 억제제를 포함하는 코로나바이러스 감염 또는 감염 질환의 예방 또는 소독용 조성물
CN113831353A (zh) * 2021-06-03 2021-12-24 四川大学 一种vegfr3小分子抑制剂及其在抗肿瘤药物中的应用
JP2024522594A (ja) 2021-06-23 2024-06-21 ギリアード サイエンシーズ, インコーポレイテッド ジアシルグリセロールキナーゼ調節化合物
AU2022299051A1 (en) 2021-06-23 2023-12-07 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
WO2022271659A1 (fr) 2021-06-23 2022-12-29 Gilead Sciences, Inc. Composés modulant les diacylglycérol kinases
AU2022297373A1 (en) 2021-06-23 2024-01-04 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
CN115716840B (zh) * 2021-08-24 2024-07-23 昆药集团股份有限公司 一种具有kras突变蛋白抑制作用的杂环化合物及其药物组合和用途
CA3234909A1 (fr) 2021-10-28 2023-05-04 Gilead Sciences, Inc. Derives de pyridine-3(2h)-one
KR20240097895A (ko) 2021-10-29 2024-06-27 길리애드 사이언시즈, 인코포레이티드 Cd73 화합물
CA3234336A1 (fr) * 2021-10-29 2023-05-04 Voronoi Inc. Compose derive quinazoline et son utilisation
CA3237577A1 (fr) 2021-12-22 2023-06-29 Gilead Sciences, Inc. Agents de degradation des doigts de zinc de la famille ikaros et leurs utilisations
EP4452414A2 (fr) 2021-12-22 2024-10-30 Gilead Sciences, Inc. Agents de dégradation de doigt de zinc de la famille ikaros et utilisations associées
TW202340168A (zh) 2022-01-28 2023-10-16 美商基利科學股份有限公司 Parp7抑制劑
WO2023178181A1 (fr) 2022-03-17 2023-09-21 Gilead Sciences, Inc. Agents de dégradation des doigts de zinc de la famille ikaros et leurs utilisations
CN114573591B (zh) * 2022-04-16 2023-04-25 成都施贝康生物医药科技有限公司 一种取代的吡咯并嘧啶化合物及其应用
WO2023205719A1 (fr) 2022-04-21 2023-10-26 Gilead Sciences, Inc. Composés modulateurs de kras g12d
US20240116928A1 (en) 2022-07-01 2024-04-11 Gilead Sciences, Inc. Cd73 compounds
WO2024137852A1 (fr) 2022-12-22 2024-06-27 Gilead Sciences, Inc. Inhibiteurs de prmt5 et leurs utilisations
WO2024215754A1 (fr) 2023-04-11 2024-10-17 Gilead Sciences, Inc. Composés modulateurs de kras
WO2024220917A1 (fr) 2023-04-21 2024-10-24 Gilead Sciences, Inc. Inhibiteurs de prmt5 et leurs utilisations

Family Cites Families (105)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3037980A (en) * 1955-08-18 1962-06-05 Burroughs Wellcome Co Pyrrolopyrimidine vasodilators and method of making them
US5710158A (en) * 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
GB9323290D0 (en) * 1992-12-10 1994-01-05 Zeneca Ltd Quinazoline derivatives
WO1997027199A1 (fr) * 1996-01-23 1997-07-31 Novartis Ag Pyrrolopyrimidines et leurs procedes de preparation
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
EP1255536B1 (fr) 1999-12-22 2006-06-28 Sugen, Inc. DERIVES D'INDOLINONE DESTINES A LA MODULATION DE LA TYROSINE PROTEINE KINASE DE TYPE c-KIT
GB0100620D0 (en) * 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical cokpounds V
GB0115393D0 (en) * 2001-06-23 2001-08-15 Aventis Pharma Ltd Chemical compounds
WO2003057149A2 (fr) 2001-12-28 2003-07-17 Bayer Corporation Heteropyrimidines et hetero-4-pyrimidones fusionnees substituees en position 4, compositions pharmaceutiques les contenant et leur utilisation dans le traitement ou la prevention de maladies et de troubles a mediation par de7¿b?
US20040171062A1 (en) 2002-02-28 2004-09-02 Plexxikon, Inc. Methods for the design of molecular scaffolds and ligands
KR102008768B1 (ko) 2002-09-06 2019-08-08 인설트 테라페틱스, 인코퍼레이티드 공유결합된 치료제 전달을 위한 사이클로덱스트린-기초 중합체
CA2503905A1 (fr) 2002-09-16 2004-03-25 Plexxikon, Inc. Structure cristalline de la proteine kinase pim-1
US20050048573A1 (en) 2003-02-03 2005-03-03 Plexxikon, Inc. PDE5A crystal structure and uses
WO2004078923A2 (fr) 2003-02-28 2004-09-16 Plexxikon, Inc. Structure cristalline de pyk2 et ses utilisations
WO2004092123A2 (fr) 2003-04-10 2004-10-28 Microbia, Inc. Inhibiteurs d'invasion fongique
US7253166B2 (en) * 2003-04-22 2007-08-07 Irm Llc 6-phenyl-7H-pyrrolo[2,3-d]pyrimidine compounds that induce neuronal differentiation in embryonic stem cells
US20050079548A1 (en) 2003-07-07 2005-04-14 Plexxikon, Inc. Ligand development using PDE4B crystal structures
US7202266B2 (en) 2003-07-17 2007-04-10 Plexxikon, Inc. PPAR active compounds
US7348338B2 (en) 2003-07-17 2008-03-25 Plexxikon, Inc. PPAR active compounds
US20050164300A1 (en) 2003-09-15 2005-07-28 Plexxikon, Inc. Molecular scaffolds for kinase ligand development
AU2004293026B2 (en) * 2003-11-21 2012-01-19 Array Biopharma Inc. AKT protein kinase inhibitors
US7517970B2 (en) 2003-12-19 2009-04-14 Plexxikon, Inc. Nucleic acids encoding kinase and phosphatase enzymes, expression vectors and cells containing same
US20070066641A1 (en) 2003-12-19 2007-03-22 Prabha Ibrahim Compounds and methods for development of RET modulators
PL1696920T3 (pl) 2003-12-19 2015-03-31 Plexxikon Inc Związki i sposoby opracowywania modulatorów Ret
US20050239806A1 (en) * 2004-01-13 2005-10-27 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
GB0403606D0 (en) 2004-02-18 2004-03-24 Novartis Ag Organic compounds
AU2005249380C1 (en) * 2004-04-23 2012-09-20 Exelixis, Inc. Kinase modulators and methods of use
US7585859B2 (en) 2004-05-06 2009-09-08 Plexxikon, Inc. PDE4B inhibitors and uses therefor
CA2570817A1 (fr) 2004-06-17 2006-01-26 Plexxikon, Inc. Composes modulant l'activite de c-kit
US7498342B2 (en) 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
EP1786813A2 (fr) 2004-09-03 2007-05-23 Plexxikon, Inc. Inhibiteurs de la phosphodiesterase 4b (pde4b)
WO2006060456A2 (fr) 2004-11-30 2006-06-08 Plexxikon, Inc. Composes actifs sur les ppar
WO2006060535A2 (fr) 2004-11-30 2006-06-08 Plexxikon, Inc. Composes actifs ppar
US20060160135A1 (en) 2004-12-08 2006-07-20 Weiru Wang SF-1 and LRH-1 modulator development
CA2590961C (fr) 2004-12-28 2013-11-26 Exelixis, Inc. Composes piperazine ou [1h-pyrazolo[3,4-d]pyrimidin-4-yl]-piperidine utilises en tant que modulateurs des serine-theoronine kinases (p70s6k, atk1 et atk2) pour le traitement de maladies immunologiques, inflammatoires et proliferantes
EP1846396A2 (fr) 2005-02-11 2007-10-24 Freie Universität Berlin 4-(indol-3-yl)chinazolines substituees et leur utilisation
WO2006091450A1 (fr) * 2005-02-18 2006-08-31 Lexicon Genetics Incorporated Composes 4-piperidin-1-yl-7h-pyrrolo[2,3-d]pyrimidine
NZ563444A (en) 2005-05-17 2011-04-29 Plexxikon Inc Pyrrolo(2,3-b)pyridine derivatives as protein kinase inhibitors
US7863288B2 (en) 2005-06-22 2011-01-04 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
EP1943245A2 (fr) 2005-09-07 2008-07-16 Plexxikon, Inc. Dérivés d'indole disubstitué en 1,3 pour utilisation comme composés agissant sur les ppar
US20080234349A1 (en) 2005-09-07 2008-09-25 Jack Lin PPAR active compounds
KR20080042170A (ko) 2005-09-07 2008-05-14 플렉시콘, 인코퍼레이티드 Ppar 활성 화합물
BRPI0708779A2 (pt) 2006-03-11 2011-06-14 Vernalis R & D derivados de pirrolopirimidina utilizados como inibidores de hsp90
US7807671B2 (en) 2006-04-25 2010-10-05 Bristol-Myers Squibb Company Diketo-piperazine and piperidine derivatives as antiviral agents
WO2008005368A2 (fr) * 2006-06-30 2008-01-10 Abbott Laboratories Pipérazines en tant qu'antagonistes de p2x7
WO2008020302A2 (fr) 2006-08-17 2008-02-21 Pfizer Products Inc. Composés hétéro-aromatiques à base de quinoline
WO2008063888A2 (fr) 2006-11-22 2008-05-29 Plexxikon, Inc. Composés modulant l'activité de c-fms et/ou de c-kit et utilisations associées
CN101641351A (zh) 2006-12-21 2010-02-03 普莱希科公司 用于激酶调节的化合物和方法及其适应症
PE20121126A1 (es) 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
WO2008079909A1 (fr) 2006-12-21 2008-07-03 Plexxikon, Inc. Composés et méthodes de modulation des kinases, et indications connexes
MX2009009290A (es) 2007-03-08 2009-09-10 Plexxikon Inc Compuestos activos en ppar.
PE20090159A1 (es) 2007-03-08 2009-02-21 Plexxikon Inc COMPUESTOS DERIVADOS DE ACIDO INDOL-PROPIONICO COMO MODULADORES PPARs
AU2008240188A1 (en) * 2007-04-13 2008-10-23 Supergen, Inc. Axl kinase inhibitors useful for the treatment of cancer or hyperproliferative disorders
UA99284C2 (ru) 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ
US8618121B2 (en) 2007-07-02 2013-12-31 Cancer Research Technology Limited 9H-pyrimido[4,5-B]indoles, 9H-pyrido[4',3':4,5]pyrrolo[2,3-D]pyridines, and 9H 1,3,6,9 tetraaza-fluorenes as CHK1 kinase function inhibitors
AU2008276063B2 (en) 2007-07-17 2013-11-28 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
WO2009021169A2 (fr) * 2007-08-08 2009-02-12 Lexicon Pharmaceuticals, Inc. Inhibiteurs de kinase, compositions les contenant et procédés d'utilisation
JP5439377B2 (ja) * 2007-09-14 2014-03-12 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ ヒスタミンh4受容体のチエノ−及びフロ−ピリミジン調節物質
EA018716B1 (ru) 2007-10-29 2013-10-30 Натко Фарма Лимитед Новые 4-(тетразол-5-ил) хиназолиновые производные в качестве противораковых средств
US20090118276A1 (en) * 2007-11-02 2009-05-07 Wyeth Thienopyrimidines, thienopyridines, and pyrrolopyrimidines as b-raf inhibitors
GB0725103D0 (en) * 2007-12-21 2008-01-30 Glaxo Group Ltd Novel compounds
KR101706391B1 (ko) * 2008-04-21 2017-02-13 렉시컨 파마슈티컬스 인코퍼레이티드 Limk2 억제제, 그를 포함하는 조성물 및 그의 사용 방법
PE20091846A1 (es) 2008-05-19 2009-12-16 Plexxikon Inc DERIVADOS DE PIRROLO[2,3-d]-PIRIMIDINA COMO MODULADORES DE CINASAS
WO2009143018A2 (fr) 2008-05-19 2009-11-26 Plexxikon, Inc. Composés et procédés de modulation des kinases, et indications associées
WO2009152087A1 (fr) 2008-06-10 2009-12-17 Plexxikon, Inc. Composés hétéroaryles bicycliques et procédés destinés à la modulation de kinases, et des indications pour celle-ci
AU2009257635A1 (en) 2008-06-10 2009-12-17 Plexxikon, Inc. 5H-Pyrrolo [2,3-b] pyrazine derivatives for kinase modulation, and indications therefor
WO2010036316A1 (fr) 2008-09-24 2010-04-01 Yangbo Feng Composés d’urée et de carbamate et analogues utilisés comme inhibiteurs de kinase
SG172259A1 (en) 2008-12-19 2011-07-28 Genentech Inc Heterocyclic compounds and methods of use
RU2011141123A (ru) 2009-03-11 2013-04-20 Плексксикон, Инк. ПРОИЗВОДНЫЕ ПИРРОЛО[2,3-b]ПИРИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ RAF-КИНАЗ
US8129404B2 (en) 2009-03-11 2012-03-06 Plexxikon Inc. Compounds and uses thereof
WO2010111527A1 (fr) 2009-03-26 2010-09-30 Plexxikon, Inc. Pyrazolo [ 3, 4 -b] pyridines en tant qu'inhibiteurs de la kinase et leur utilisation médicale
EP2414356B1 (fr) 2009-04-03 2015-09-02 F.Hoffmann-La Roche Ag Compositions de {3-[5-(4-chlorophényl)-1h-pyrrolo(2,3-b)pyridine-3-carbonyl]-2,4-difluorophényl)}-amide de l'acide propane-1-sulfonique et leurs utilisations
MX2011011735A (es) 2009-05-04 2011-11-29 Plexxikon Inc Compuestos y metodos para la inhibicion de renina, e indicaciones para ello.
TW201041888A (en) 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
CA2767079A1 (fr) * 2009-07-08 2011-01-13 Leo Pharma A/S Composes heterocycliques en tant qu'inhibiteurs du recepteur jak et de la proteine tyrosine kinase
CA2773131C (fr) * 2009-09-04 2015-07-14 The Regents Of The University Of Michigan Compositions et methodes de traitement de la leucemie
MX2012005284A (es) 2009-11-06 2012-06-28 Plexxikon Inc Compuestos y metodos para la modulacion de cinasas. e indicaciones para ello.
KR20120097512A (ko) 2009-11-18 2012-09-04 플렉시콘, 인코퍼레이티드 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증
AU2010336524B2 (en) 2009-12-23 2015-10-08 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
TWI619713B (zh) 2010-04-21 2018-04-01 普雷辛肯公司 用於激酶調節的化合物和方法及其適應症
CA2761074A1 (fr) * 2010-05-05 2011-11-10 Vertex Pharmaceuticals Incorporated Pyrazolopyrimidines 4-substituees pouvant etre employees en tant qu'inhibiteurs de pkc-theta
US8642606B2 (en) 2010-09-29 2014-02-04 Plexxikon Inc. ZAP-70 active compounds
JP5927201B2 (ja) 2010-12-16 2016-06-01 カルチャン リミテッド Ask1阻害ピロロピリミジン誘導体
CN103328482A (zh) * 2011-01-03 2013-09-25 韩美药品株式会社 用于调节g蛋白-偶联受体的新双环化合物
EA028821B9 (ru) 2011-02-07 2018-10-31 Плексксикон, Инк. Соединения и способы для модуляции киназ, а также показания к их применению
AR085279A1 (es) 2011-02-21 2013-09-18 Plexxikon Inc Formas solidas de {3-[5-(4-cloro-fenil)-1h-pirrolo[2,3-b]piridina-3-carbonil]-2,4-difluor-fenil}-amida del acido propano-1-sulfonico
BR112013029163A2 (pt) 2011-05-17 2017-01-31 Plexxikon Inc modulação quinase e indicações dos mesmos
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
CA2881901C (fr) * 2012-08-31 2017-10-10 Novadrug, Llc Carboxamides heterocyclyle pour le traitement de maladies virales
PT2935248T (pt) 2012-12-21 2018-04-05 Plexxikon Inc Compostos e métodos para a modulação de quinase e indicações associadas
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
AU2014233437B2 (en) 2013-03-15 2018-07-26 Opna Immuno Oncology, SA Heterocyclic compounds and uses thereof
EP3004060B1 (fr) 2013-05-30 2019-11-27 Plexxikon Inc. Composés pour modulation de kinases, et indications correspondantes
US9771369B2 (en) 2014-03-04 2017-09-26 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
WO2016044067A1 (fr) 2014-09-15 2016-03-24 Plexxikon Inc. Composés hétérocycliques et leurs utilisations
WO2016164641A1 (fr) 2015-04-08 2016-10-13 Plexxikon Inc. Composés et méthodes de modulation des kinases, et leurs indications
EP3581573B1 (fr) 2015-05-06 2022-07-06 Plexxikon Inc. Synthèse d'un composé modulant des kinases
ES2820827T3 (es) 2015-05-06 2021-04-22 Plexxikon Inc Formas sólidas de un compuesto modulador de quinasas
US10316032B2 (en) 2015-05-22 2019-06-11 Plexxikon Inc. Solid forms of a compound for modulating kinases
CN107801378A (zh) 2015-05-22 2018-03-13 普莱希科公司 用于治疗braf‑v600相关的疾病的plx‑8394或plx‑7904
WO2017019804A2 (fr) 2015-07-28 2017-02-02 Plexxikon Inc. Composés et procédés de modulation des kinases, et indications associées
KR20180052757A (ko) 2015-09-21 2018-05-18 플렉시콘 인코퍼레이티드 헤테로시클릭 화합물 및 그의 용도
WO2017100201A1 (fr) 2015-12-07 2017-06-15 Plexxikon Inc. Composés et procédés pour la modulation de kinase, et indications associées
CA3017972C (fr) 2016-03-16 2023-03-28 Plexxikon Inc. Composes et procedes de modulation de kinases et indications associees

Also Published As

Publication number Publication date
WO2014039714A2 (fr) 2014-03-13
JP2015529224A (ja) 2015-10-05
ES2889757T3 (es) 2022-01-13
EP2892534A2 (fr) 2015-07-15
MX2015002887A (es) 2015-07-06
EP2892534B8 (fr) 2021-09-15
EP2892534B1 (fr) 2021-08-04
AU2013312477A1 (en) 2015-04-02
US20140128390A1 (en) 2014-05-08
AU2013312477B2 (en) 2018-05-31
CA2883894C (fr) 2020-08-18
JP6318156B2 (ja) 2018-04-25
WO2014039714A3 (fr) 2014-10-02
CN104981247A (zh) 2015-10-14
US10227357B2 (en) 2019-03-12

Similar Documents

Publication Publication Date Title
CA2883894C (fr) Composes et procedes pour la modulation des kinases, et leurs indications
EP2935248B1 (fr) Composés et procédés pour la modulation de kinase, et indications associées
AU2014233437B2 (en) Heterocyclic compounds and uses thereof
CA2961356C (fr) Composes heterocycliques et utilisations dans la modulation du bromodomaine et le traitement des maladies ou conditions connexes
WO2015134536A1 (fr) Composés et méthodes de modulation des kinases, et leurs indications
CA2912568A1 (fr) Composes pour modulation de kinases, et indications correspondantes

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20180705